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Polycrystalline methacryloyl monomers of the antibacterial drug nalidixic acid with an anhydride bond to the drug carboxyl group were prepared. The physicochemical properties of the synthesized vinyl monomer were characterized using X-ray powder diffraction, thermal analysis, and polarized light microscopy measurements. Mechanochemical solid-state polymerization of the resulting monomers was carried out to yield a novel polymeric prodrug. The in vitro hydrolysis behavior of the polymeric prodrug indicated that the release rate of drug from the polymeric prodrug was clearly dependent on the pH value of the hydrolysis solution. Moreover, sustained release of the drug at an almost constant rate for more than 10 hr was shown in both neutral and alkaline solutions. The results suggest that anhydride-based polymeric prodrugs could be potentially useful in colon targeted drug delivery systems.
Assuntos
Anidridos/química , Antibacterianos/química , Metacrilatos/química , Ácido Nalidíxico/química , Polímeros/química , Pró-Fármacos/química , Liberação Controlada de Fármacos , Humanos , Hidrólise , Polimerização , PósRESUMO
A detailed electron spin resonance (ESR) analysis of mechanically induced free radicals (mechanoradicals) formation of glucose-based polysaccharides, dextran (Dx) and glycogen (Gly) was performed in comparison with amylose mechanoradicals. The ESR spectra of the samples mechanically fractured at room temperature were multicomponent. The radical concentration of Dx and Gly mechanoradicals gradually decreased during vibratory milling after reaching the maximum value. Although the molecular weight of Dx or the particle diameter of Gly steeply diminished until reaching the each maximum value of radical concentration, after that the molecular weight or the particle diameter slowly decreased. These results suggested that Dx and Gly mechanoradicals might be more unstable than amylose radicals possessing an intramolecular helical structure due to the branched structure.
RESUMO
Novel polymeric prodrugs were synthesized by mechanochemical solid-state copolymerization of hydroxyethylcellulose and the methacryloyloxy derivative of 5-fluorouracil (5-FU). Copolymerization was about 94% complete after 4 h, and the polymeric prodrug was quantitatively obtained after 14 h of reaction. The number average molecular weight (Mn) and polydispersity (H) of the polymeric prodrug were 39000 g/mol and 6.20, respectively. Mechanical fracturing of the polymer in a stainless steel twin-shell blender improved these properties (Mn=16000 g/mol and H=1.94). 5-FU was sustainably released from the polymeric prodrugs, and the rate was not affected by the molecular weight or molecular weight distribution of the prodrug under the experimental conditions used. These results suggest that novel polymeric prodrugs composed of a polysaccharide and a synthetic polymer can be fabricated by mechanochemical solid-state copolymerization under anaerobic conditions.
Assuntos
Celulose/análogos & derivados , Polímeros/síntese química , Pró-Fármacos/síntese química , Compostos de Vinila/química , Celulose/química , Hidrólise , Fenômenos Mecânicos , Estrutura Molecular , Peso Molecular , Polimerização , Polímeros/química , Pró-Fármacos/químicaRESUMO
BACKGROUND: The hallux plays a crucial role in maintaining standing balance and facilitating forward and backward movements during gait. CASE PRESENTATION: A 21-year-old Japanese patient, suffering from a traumatic hallux deficit with only a portion of the basal phalanx intact, underwent rehabilitation treatment. The thenar area exhibited instability, leading to impaired balance and walking difficulties. Biomechanical assessment revealed the need for a rehabilitation strategy for the foot, as well as the knee, hip, and trunk. A rehabilitation protocol was designed to enhance medial foot loading during walking and standing, including balance and trunk strength training. After a 12-week rehabilitation period, the patient's gait showed significant improvement. Specifically, the load response and single-support phases of the gait cycle on the affected side increased from 46.9% to 49.3%, while the pre-swing phase decreased from 14.6% to 11.6%. The vertical component of the ground reaction force rose from 599.8 to 647.5 N. The enhanced stability from balance training and increased muscle strength contributed to the patient's improved walking and balance. CONCLUSION: A patient with a traumatic hallux deficit underwent conservative treatment through strategic rehabilitation according to biomechanical assessment. This case report underscores the value of biomechanical gait analysis in the conservative management of similar conditions.
Assuntos
Hallux , Medicina , Adulto , Humanos , Adulto Jovem , Pé , Análise da Marcha , Extremidade Inferior , CaminhadaRESUMO
Dextran (Dx) is a biodegradable and biocompatible polysaccharide, thus promising as a drug delivery carrier for tumor therapy. Herein, we applied mechanical energy to a high molecular weight Dx to control its molecular weight and simultaneously generate mechanoradicals. The solid-state polymerization of methacrylate- or methacrylamide derivatives initiated with Dx mechanoradicals showed polymer conversion of >95%, yielding Dx-based graft copolymers with molecular weights of approximately 30,000 g mol-1. The Dx-based graft copolymers with hydrophobic segments formed nanoparticles with a particle size of 25-35 nm in an aqueous solution. The anti-pancreatic tumor drug 5-fluorouracil (5-FU) was covalently conjugated onto the hydrophobic segments of the amphiphilic Dx, and the nanoparticles were also prepared. The drug release profile from 5-FU-conjugated nanoparticles corresponded well to the Korsmeyer-Peppas model applied to drug release from matrix substrates, and was also immensely predicted by the Logistic and Gompertz curves. The 5-FU-conjugated nanoparticles showed cytotoxicity against the pancreatic adenocarcinoma cell lines (BxPC-3) that were not significantly inferior to the 5-FU positive group. Furthermore, the fluorescein-labeled nanoparticles internalized into BxPC-3 within 6 h and actively migrated into the cytosol. These results suggest that Dx-based graft copolymers with hydrophobic segments might be used to enhance therapeutic activity.
Assuntos
Dextranos , Portadores de Fármacos , Fluoruracila , Nanopartículas , Polimerização , Fluoruracila/química , Fluoruracila/farmacologia , Dextranos/química , Humanos , Nanopartículas/química , Linhagem Celular Tumoral , Portadores de Fármacos/química , Portadores de Fármacos/síntese química , Ácidos Polimetacrílicos/química , Ácidos Polimetacrílicos/síntese química , Liberação Controlada de Fármacos , Sistemas de Liberação de Medicamentos , Interações Hidrofóbicas e Hidrofílicas , Tamanho da PartículaRESUMO
Background: Little League elbow, including humeral epicondylitis and osteochondritis dissecans, is a severe throwing injury in school-aged pitchers. Recent rule revisions have been implemented, and thus, prevention awareness may have increased. Purpose: To compare the incidence of elbow injury in 2011 from a previous study with that in 2021 and examine changes in the incidence and characteristics of players with elbow injuries. Study Design: Cross-sectional study; Level of evidence, 3. Methods: A survey based on the 2011 survey was conducted from September 1 to December 31, 2021, among 4060 third- to sixth-grade Little League players belonging to 203 teams in Kyoto, Japan. This survey included a 23-item checklist on physical condition and injury. The participants were classified into 2 groups according to the presence or absence of an elbow injury in the dominant arm during the season. The Wilcoxon rank-sum test was conducted to compare differences in basic information between the 2 groups. We also compared the differences in the 23 checklist items between the 2 groups using the chi-square or Fisher exact probability test. Results: Overall, 98 teams (1335 players; age range, 8-12 years) returned the questionnaires (collection rate, 32.9%). The final analysis population (excluding incomplete questionnaires) was 678 (mean age, 10.6 ± 1.1 years). Elbow injuries accounted for 30.7% of all injury sites in the players. Overall, 61 players (9.0%) reported elbow injuries in 2021 compared with 19.1% of the players in the 2011 survey (P < .01) A significantly higher percentage of players with elbow injuries had elbow pain in extension (item 2 on the survey checklist, P < .001) and flexion (item 4, P < .0024), were regular players (item 5, P = .0288), played baseball under fatigue (item 8, P = .0028), and had lower and upper limb inflexibility (item 17, P = .0379; item 18, P = .0146; and item 22, P = .0085). Conclusion: Study findings indicated that the incidence of elbow injuries has decreased significantly over the past 10 years, although the elbow joint still accounted for almost one-third of all injuries in Japanese youth baseball players.
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BACKGROUND: Anterior cruciate ligament (ACL) injuries are among the most common injuries in the National Basketball Association (NBA), and it is important to investigate the actual nature of the injury because it can impair a player's performance after returning to the game. Although the moment of injury has been investigated, the details of the movements and circumstances leading to injury in basketball games are unknown. This study aimed to clarify the actions leading to ACL injuries and to investigate their characteristics, based on YouTube video analyses of the NBA players. METHODS: Players with ACL injuries in the NBA were identified through web-based research over 10 seasons (2011/2012-2021/2022, through October 2021), with 29 recorded videos of ACL injuries in the NBA. Actions were categorized based on basketball-specific gestures, and determined whether the player was in contact with an opponent or not and, if so, the location of the contact was analyzed focusing on two time points: at the injury frame (IF) and one step before the injury frame (IF-1). The "injury leg" timing was counted for each of the first and second steps after ball possession. RESULTS: The majority (68.2%) of ACL injury occurred during the 2 steps phase (only two steps can proceed after ball retention in basketball, so we defined them as two steps) in the offense action, and most notably during the first step (80.0%). 73.3% of players who were injured during the 2 steps phase got contact to an area other than the knee (Indirect contact) at the IF-1, with 81.8% of contact being located in the upper body contralateral to the respective knee injury. The probability of players with ACL injuries during the 2 steps at the IF-1 who got Indirect contact was statistically significantly greater than those who got no contact with other players (p = 0.042). CONCLUSIONS: We argue that including pre-injury play and contact falls into the novelty category. Through YouTube-based video analyses, this study revealed that ACL injuries tend to be characterized by specific types of actions, the timing of contact, and the location of contact in NBA players.
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INTRODUCTION: High heeled shoes have long been worn in society and they are known to cause biomechanical imbalances to not only the foot, but the whole musculoskeletal system. This study aims to show the detailed changes that happen to the shape of the transverse arch of the foot in high heels, using two different inclination degrees. METHODS: 68 women participated in this study. Two custom-made high heels were made with inclinations of 15 degrees and 30 degrees (cm). A weight-bearing ultrasound was used to assess the coronal view of the transverse arch in standing. ANOVA and Tuckey tests were used to compare the results between 0 degrees, 15 degrees and 30 degrees inclinations. RESULTS: The transverse arch height was slightly increased as the heel height increased (0DI-15DI: p = 0.5852 / 15DI-30DI: p = 0.395 / 0DI-30DI: p = 0.0593). The transverse arch length (0DI-15DI: p = 0.0486 / 15DI-30DI: p = 0.0004 / 0DI-30DI: p = 0.1105) and the area under the metatarsal heads (0DI-15DI: p = 0.0422 / 15DI-30DI: p = 0.0180 / 0DI-30DI: p = 0.9463) significantly decreased as the heel height increased. DISCUSSION: The main changes were viewed in the 30 degrees inclinations compared to 0 degrees inclination. When the toes are dorsiflexed in high heels, it stimulates the Windlass mechanism which in turn stiffens the plantar fascia and adducts the metatarsal heads, while the soft tissues shrink in response to loads. CONCLUSION: High heels affected the shape of the transverse arch even in short term standing, and these effects increased as the height of the heel increased.